基本信息:
- 专利标题： KINASE MODULATORS AND METHODS OF USE
- 专利标题（中）：激酶调节剂及其使用方法
- 申请号：PCT/US2005/013860 申请日：2005-04-22
- 公开(公告)号：WO2005117909A2 公开(公告)日：2005-12-15
- 发明人： ANAND, Neel, K. , BLAZEY, Charles, M. , BOWLES, Owen, Joseph , BUSSENIUS, Joerg , CANNE BANNEN, Lynne , CHAN, Diva Sze-Ming , CHEN, Baili , CO, Erick Wang , COSTANZO, Simona , DEFINA, Steven, Charles , DUBENKO, Larisa , FRANZINI, Maurizio , HUANG, Ping , JAMMALAMADAKA, Vasu , KHOURY, Richard George , KIM, Moon, Hwan , KLEIN, Rhett, Ronald , LE, Donna, Tra , MAC, Morrison, B. , NUSS, John, M. , PARKS, Jason, Jevious , RICE, Kenneth, D. , TSANG, Tsze, H. , TSUHAKO, Amy, Lew , WANG, Yong , XU, Wei
- 申请人： EXELIXIS, INC. , ANAND, Neel, K. , BLAZEY, Charles, M. , BOWLES, Owen, Joseph , BUSSENIUS, Joerg , CANNE BANNEN, Lynne , CHAN, Diva Sze-Ming , CHEN, Baili , CO, Erick Wang , COSTANZO, Simona , DEFINA, Steven, Charles , DUBENKO, Larisa , FRANZINI, Maurizio , HUANG, Ping , JAMMALAMADAKA, Vasu , KHOURY, Richard George , KIM, Moon, Hwan , KLEIN, Rhett, Ronald , LE, Donna, Tra , MAC, Morrison, B. , NUSS, John, M. , PARKS, Jason, Jevious , RICE, Kenneth, D. , TSANG, Tsze, H. , TSUHAKO, Amy, Lew , WANG, Yong , XU, Wei
- 申请人地址： P. O. Box 511, 170 Harbor Way, South San Francisco, CA 94083-0511 US
- 专利权人： EXELIXIS, INC.,ANAND, Neel, K.,BLAZEY, Charles, M.,BOWLES, Owen, Joseph,BUSSENIUS, Joerg,CANNE BANNEN, Lynne,CHAN, Diva Sze-Ming,CHEN, Baili,CO, Erick Wang,COSTANZO, Simona,DEFINA, Steven, Charles,DUBENKO, Larisa,FRANZINI, Maurizio,HUANG, Ping,JAMMALAMADAKA, Vasu,KHOURY, Richard George,KIM, Moon, Hwan,KLEIN, Rhett, Ronald,LE, Donna, Tra,MAC, Morrison, B.,NUSS, John, M.,PARKS, Jason, Jevious,RICE, Kenneth, D.,TSANG, Tsze, H.,TSUHAKO, Amy, Lew,WANG, Yong,XU, Wei
- 当前专利权人： EXELIXIS, INC.,ANAND, Neel, K.,BLAZEY, Charles, M.,BOWLES, Owen, Joseph,BUSSENIUS, Joerg,CANNE BANNEN, Lynne,CHAN, Diva Sze-Ming,CHEN, Baili,CO, Erick Wang,COSTANZO, Simona,DEFINA, Steven, Charles,DUBENKO, Larisa,FRANZINI, Maurizio,HUANG, Ping,JAMMALAMADAKA, Vasu,KHOURY, Richard George,KIM, Moon, Hwan,KLEIN, Rhett, Ronald,LE, Donna, Tra,MAC, Morrison, B.,NUSS, John, M.,PARKS, Jason, Jevious,RICE, Kenneth, D.,TSANG, Tsze, H.,TSUHAKO, Amy, Lew,WANG, Yong,XU, Wei
- 当前专利权人地址： P. O. Box 511, 170 Harbor Way, South San Francisco, CA 94083-0511 US
- 代理机构： ATKINS, Michael, J.
- 优先权： US60/564,908 20040423
- 主分类号： A61K31/7076
- IPC分类号： A61K31/7076
摘要：
The present invention relates to compounds of the Formula I and II wherein R, R 21 , R 25 -R 33 , m, n, X 21 -X 23 , and Q 1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要（中）：
本发明涉及式I和II的化合物，其中R，R 21，R 25 -R 33，m，n，X 21-X 23和Q 1在本文中定义。 该化合物调节蛋白激酶酶活性以调节细胞活性，如增殖，分化，程序性细胞死亡，迁移和化学侵袭。 本发明的化合物抑制，调节和/或调节激酶，特别是p70S6和/或Akt激酶。 使用和制备化合物的方法及其药物组合物治疗激酶依赖性疾病和病症也是本发明的一个方面。
IPC结构图谱:
| A | 人类生活必需 |
| --A61 | 医学或兽医学；卫生学 |
| ----A61K | 医用、牙科用或梳妆用的配制品 |
| ------A61K31/00 | 含有机有效成分的医药配制品 |
| --------A61K31/70 | .碳水化合物；糖；其衍生物 |
| ----------A61K31/7028 | ..含有通过配糖键与非糖化合物连接的糖基的化合物 |
| ------------A61K31/7052 | ...含有氮作为环杂原子的，例如核苷、核苷酸 |
| --------------A61K31/706 | ....含有氮作为环杂原子的六元环的 |
| ----------------A61K31/7064 | .....含有稠合或非稠合的嘧啶的 |
| ------------------A61K31/7076 | ......含嘌呤的，例如腺苷、腺苷磷酸 |